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Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis
Authors:Meng Charles Q  Somers Patricia K  Rachita Carolyn L  Holt Lisa A  Hoong Lee K  Zheng X Sharon  Simpson Jacob E  Hill Russell R  Olliff Lynda K  Kunsch Charles  Sundell Cynthia L  Parthasarathy Sampath  Saxena Uday  Sikorski James A  Wasserman Martin A
Institution:AtheroGenics, Inc., 8995 Westside Parkway, GA 30004, Alpharetta, USA. cmeng@atherogenics.com
Abstract:A series of novel phenolic compounds has been discovered as potent inhibitors of TNF-alpha-inducible expression of vascular cell adhesion molecule-1 (VCAM-1) with concurrent antioxidant and lipid-modulating properties. Optimization of these multifunctional agents led to the identification of 3a (AGI-1067) as a clinical candidate with demonstrated efficacies in animal models of atherosclerosis and hyperlipidemia.
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